[CAS NO. 3033615-55-0] GLS1 Inhibitor-6
PRODUCTS SPECIFICATIONS [3033615-55-0]
DESCRIPTION [3033615-55-0]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 660.91 |
| Molecular Formula | C37H52N6O3S |
| SMILES | O=C(NCC1CCN(CCCCCC)CC1)C2=CC=CC(COCCC3CCN(C4=NN=C(NC(CC5=CC=CC=C5)=O)S4)CC3)=C2 |
Summary
GLS1 Inhibitor-6 (Compound 24y) is an orally active, potent and selective glutaminase 1 ( GLS1 ) inhibitor ( IC 50 =68 nM), shows 220-fold selectivity for GLS2. GLS1 Inhibitor-6 shows good anti-tumor activity, antitumor cell proliferation activity and induces apoptosis [1] .
IC50 & Target
IC50: 68 nM (GLS1) [1]
In Vitro
GLS1 Inhibitor-6 (0-10 μM) inhibts cancer cell growth
[1]
.
GLS1 Inhibitor-6 (1-10 μM, 48 h) can induce A549 cell apoptosis
[1]
.
GLS1 Inhibitor-6 (50-800 nM, 48 h) can induce cell cycle arrest in the G1 phase
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| Cell Line: | A549 and HCT116 cell |
| Concentration: | 0-10 μM |
| Incubation Time: | |
| Result: | Inhibited A549 and HCT116 cell growth with IC 50 s of 0.57 and 0.42 μM, respectively. |
Apoptosis Analysis [1]
| Cell Line: | A549 cell |
| Concentration: | 1, 5, and 10 μM |
| Incubation Time: | 48 h |
| Result: | Showed the population of apoptotic cells to 84% at the concentration of 10 μM. |
Cell Cycle Analysis [1]
| Cell Line: | A549 cell |
| Concentration: | 50, 100, 200, 400 and 800 nM |
| Incubation Time: | 48 h |
| Result: | Resulted in G1 phase cell cycle arrest in a dose-dependent manner, and decreased proportion of cells in the S phase. |
In Vivo
GLS1 Inhibitor-6 (oral gavage; 100 mg/kg; once daily; 28 d) treatment inhibits tumor growth in the preclinical mouse models [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Rats [1] | ||||||||||||||||||
| Dosage: | 3 mg/kg | ||||||||||||||||||
| Administration: | I.V. and P.O.; 3 mg/kg; once | ||||||||||||||||||
| Result: |
|
| Animal Model: | Human non-small cell lung A549 xenograft tumor model, GLS1 high-expression HCT116 xenograft tumor model [1] |
| Dosage: | 100 mg/kg |
| Administration: | Oral gavage; 100 mg/kg; once daily; 28 days |
| Result: | Showed 40.9% tumor growth inhibition in A549 model, and showed 42% tumor growth inhibition in HCT116 model. |
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.